51460-41-4Relevant academic research and scientific papers
HETEROARYL COMPOUNDS FOR KINASE INHIBITION
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Paragraph 461, (2016/04/26)
Compounds and pharmaceutical compositions that modulate kinase activity, including mutant EGFR and mutant HER2 kinase activity, and compounds, pharmaceutical compositions, and methods of treatment of diseases and conditions associated with kinase activity, including mutant EGFRand mutant HER2 activity, are described herein.
A selective, tin-free radical mediated synthesis of indoles based on a sulfonate template
Gray, Vincent James,Wilden, Jonathan D.
supporting information; experimental part, p. 41 - 44 (2012/01/05)
A synthesis of indoles based on a vinyl sulfonate template is described. The approach employs a sulfonate group which plays three discrete roles in the synthetic sequence. Firstly the highly electron-withdrawing sulfonate group behaves as an activating group for a 1,4-addition of an aniline to the unsaturated system. Secondly, the electron-withdrawing nature of the same group also allows it to behave as a radical stabilising group which facilitates radical cyclisation to an aromatic ring to yield a transient indoline. Finally, the pendant sulfonate group behaves as a leaving group to yield the indole.
